| Project/Area Number |
17K19226
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| Research Category |
Grant-in-Aid for Challenging Research (Exploratory)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Agricultural chemistry and related fields
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| Research Institution | Shizuoka University |
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Principal Investigator |
Takeuchi Jun 静岡大学, 農学部, 助教 (00776320)
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| Project Period (FY) |
2017-06-30 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥6,370,000 (Direct Cost: ¥4,900,000、Indirect Cost: ¥1,470,000)
Fiscal Year 2019: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2018: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Fiscal Year 2017: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
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| Keywords | 植物 / 有機化学 / 生理活性 |
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| Outline of Final Research Achievements |
Signaling by the plant stress hormone abscisic acid (ABA) is triggered by activation of PYR/PYL/RCAR receptors (PYLs). By binding to PYLs, ABA induces a conformational change associated with gate closure that enables the receptor to bind to, and inhibit, group-A protein phosphatases 2C (PP2Cs), which normally repress ABA signaling as a negative regulator. Based on this mechanism for activating the receptor, we predicted that a PYL ligand capable of switching the conformation between the gate-opened and the gate-closed forms in response to light can activate or inactivate PYLs by light irradiation. To test this prediction, LIAP/iLIAP, in which the planar vinyl methyl portion of ABA was replaced with an azobenzene group, was designed and synthesized as a photoswitchable PYL agonist/antagonist.
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| Academic Significance and Societal Importance of the Research Achievements |
人を対象とした創薬研究においては，リガンドの活性（構造変化）を光で制御した例は報告されていたが，それを植物ホルモンに適用した例はこれまでなかった。本研究で合成したLIAP/iLIAPは365 nmの光照射により90%以上がZ体（LIAP）となり，ABAと比較すると完全ではないものの，PYLの配座を活性型にするアゴニストとして機能した。また，Z体は自然条件下で徐々に安定型であるE体（iLIAP）に戻っていき，E体はPYLの配座を不活性型にするアンタゴニストとして作用した。これらの知見は，植物ホルモン受容体の活性を光によってON/OFF制御する技術基盤の構築に大きく貢献するものである。
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